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. 2024 Jan 31;13:13. doi: 10.1186/s40164-023-00468-1

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© The Author(s) 2023

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated in a credit line to the data.

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Fig. 1 — Ogremorphin is a highly specific inhibitor of GPR68. (A) Structure of OGM1 (5-ethyl-5’-(1-naphthyl)-3’H-spiro [indole-3,2’- [1, 3, 4]thiadiazole]-2-one). (B and C) Dorsal view of vehicle (DMSO)- and 10 µM OGM1-treated zebrafish embryo at 48 h post-fertilization (hpf). In contrast to the control embryo, OGM1-treated embryo showed abnormal melanocyte pigmentation, characterized by a striped pattern (blue arrow) restricted to the dorsal aspects of the embryo. (D) OGM1 only inhibited 2 GPCRs in a screen of 158 GPCRs (Data in Supplemental Table 2). (E and F) Core scaffold for OGM derivatives and structure activity relationship (SAR) analysis. Loss of LPAR1 activity did not correlate with loss of the zebrafish phenotype. Commercial inhibitor (inh) of LPAR1 (Ki16425, Sigma) also failed to recapitulate the phenotype. (G) Acidic stimulation of GPR68 expressed in HEK293 elicits a calcium response that is inhibited by OGM (N = 8). (H) Serum-responsive element-luciferase (SRE-luc) reporter by itself had low basal activity in 293T cells. Upon co-transfection with GPR4, luciferase activity increased with acidification but was not inhibited by OGM at 1, 10, or 100 µM. By contrast, when GPR68 was co-transfected with SRE-luc and stimulated by acidification, 10 µM OGM completely inhibited the signal. (n = 4, ****P < 0.0001)